Comparative Pharmacology
Head-to-head clinical analysis: APOKYN versus PERGOLIDE MESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APOKYN versus PERGOLIDE MESYLATE.
APOKYN vs PERGOLIDE MESYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Apomorphine is a non-ergoline dopamine agonist that stimulates dopamine D2 and D1 receptors. It also activates D3, D4, and D5 receptors and has some serotonergic and adrenergic activity.
Ergoline-derived dopamine D2 receptor agonist; also activates D1 and D3 receptors, and has antagonist activity at α2-adrenergic and 5-HT2B receptors.
Subcutaneous injection: 0.2 mL (2 mg) as a test dose, then 0.1-0.6 mL (1-6 mg) as needed for episodes of hypomobility; maximum single dose: 0.6 mL (6 mg); maximum daily dose: 2.0 mL (20 mg).
0.05 mg orally once daily for first 2 days, then increase by 0.1-0.15 mg/day every 3 days over 12 days, then by 0.25 mg/day every 3 days until optimal response; usual therapeutic range 2-3 mg/day divided 3 times daily; maximum 5 mg/day.
None Documented
None Documented
Terminal elimination half-life approximately 30–60 minutes (range 0.5–1 hour); clinically, rapid clearance necessitates continuous or frequent dosing for sustained effect
Terminal elimination half-life: 15-27 hours (mean 21 hours); clinically relevant for once-daily dosing
Renal (approx. 90% as metabolites and unchanged drug; <5% unchanged in urine); biliary/fecal (minor, <10%)
Renal: 50-60% as metabolites; Fecal: 40-50%; Biliary: minor (<5%)
Category C
Category C
Dopamine Agonist
Dopamine Agonist